Synthesis, structure–activity relationship, and antimalarial efficacy of 6-chloro-2-arylvinylquinolines
G Huang, C Murillo Solano, J Melendez… - Journal of medicinal …, 2020 - ACS Publications
There is an urgent need to develop new efficacious antimalarials to address the emerging
drug-resistant clinical cases. Our previous phenotypic screening identified styrylquinoline …
drug-resistant clinical cases. Our previous phenotypic screening identified styrylquinoline …
ICI 56,780 Optimization: Structure–Activity Relationship Studies of 7-(2-Phenoxyethoxy)-4(1H)-quinolones with Antimalarial Activity
JR Maignan, CL Lichorowic, J Giarrusso… - Journal of medicinal …, 2016 - ACS Publications
Though malaria mortality rates are down 48% globally since 2000, reported occurrences of
resistance against current therapeutics threaten to reverse that progress. Recently …
resistance against current therapeutics threaten to reverse that progress. Recently …
Synthesis, Antimalarial Activity, and Structure–Activity Relationship of 7-(2-Phenoxyethoxy)-4(1H)-quinolones
RM Cross, NK Namelikonda, TS Mutka… - Journal of medicinal …, 2011 - ACS Publications
ICI 56,780 (5) displayed causal prophylactic and blood schizonticidal activity (ED50= 0.05
mg/kg) in rodent malaria models but produced rapid acquisition of parasitological resistance …
mg/kg) in rodent malaria models but produced rapid acquisition of parasitological resistance …
Structure–activity relationships amongst 4-position quinoline methanol antimalarials that inhibit the growth of drug sensitive and resistant strains of Plasmodium …
E Milner, W McCalmont, J Bhonsle, D Caridha… - Bioorganic & Medicinal …, 2010 - Elsevier
Utilizing mefloquine as a scaffold, a next generation quinoline methanol (NGQM) library was
constructed to identify early lead compounds that possess biological properties consistent …
constructed to identify early lead compounds that possess biological properties consistent …
Discovery of a quinoline-4-carboxamide derivative with a novel mechanism of action, multistage antimalarial activity, and potent in vivo efficacy
B Baragaña, NR Norcross, C Wilson… - Journal of medicinal …, 2016 - ACS Publications
The antiplasmodial activity, DMPK properties, and efficacy of a series of quinoline-4-
carboxamides are described. This series was identified from a phenotypic screen against …
carboxamides are described. This series was identified from a phenotypic screen against …
Synthesis and evaluation of 7-substituted 4-aminoquinoline analogues for antimalarial activity
JY Hwang, T Kawasuji, DJ Lowes… - Journal of medicinal …, 2011 - ACS Publications
We previously reported that substituted 4-aminoquinolines with a phenyl ether substituent at
the 7-position of the quinoline ring and the capability of intramolecular hydrogen bonding …
the 7-position of the quinoline ring and the capability of intramolecular hydrogen bonding …
Discovery and structure–activity relationships of quinazolinone-2-carboxamide derivatives as novel orally efficacious antimalarials
B Laleu, Y Akao, A Ochida, S Duffy… - Journal of medicinal …, 2021 - ACS Publications
A phenotypic high-throughput screen allowed discovery of quinazolinone-2-carboxamide
derivatives as a novel antimalarial scaffold. Structure–activity relationship studies led to …
derivatives as a novel antimalarial scaffold. Structure–activity relationship studies led to …
Orally Bioavailable 6-Chloro-7-methoxy-4(1H)-quinolones Efficacious against Multiple Stages of Plasmodium
RM Cross, DL Flanigan, A Monastyrskyi… - Journal of Medicinal …, 2014 - ACS Publications
The continued proliferation of malaria throughout temperate and tropical regions of the world
has promoted a push for more efficacious treatments to combat the disease. Unfortunately …
has promoted a push for more efficacious treatments to combat the disease. Unfortunately …
Design and Synthesis of Orally Bioavailable Piperazine Substituted 4(1H)-Quinolones with Potent Antimalarial Activity: Structure–Activity and Structure–Property …
R Neelarapu, JR Maignan, CL Lichorowic… - Journal of medicinal …, 2018 - ACS Publications
Malaria deaths have been decreasing over the last 10–15 years, with global mortality rates
having fallen by 47% since 2000. While the World Health Organization (WHO) recommends …
having fallen by 47% since 2000. While the World Health Organization (WHO) recommends …
Favorable Preclinical Pharmacological Profile of a Novel Antimalarial Pyrrolizidinylmethyl Derivative of 4-amino-7-chloroquinoline with Potent In Vitro and In Vivo …
N Basilico, S Parapini, S D'Alessandro, P Misiano… - Biomolecules, 2023 - mdpi.com
The 4-aminoquinoline drugs, such as chloroquine (CQ), amodiaquine or piperaquine, are
still commonly used for malaria treatment, either alone (CQ) or in combination with …
still commonly used for malaria treatment, either alone (CQ) or in combination with …